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Curr Radiopharm ; 5(4): 348-55, 2012 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-22642421

RESUMO

D-Serine is a physiological coagonist of the N-methyl D-aspartate (NMDA) type of glutamate receptor-a key excitatory neurotransmitter receptor in the brain. D-Serine appears to be a part of the synapse through a variety of transporters located on both neurons and astrocytes. The development of 99mTc radiolabeled amino acid based radiopharmaceuticals for imaging a variety of tumors has found to be useful in diagnostic imaging. Diethylene triamine penta acetic acid (DTPA) is one of the most well-known chelating reagent for the production of stable complexes with various heavy metal ions. We have synthesized [DTPA-bis(D-ser)] in 90% yield and analyzed the chelate by spectroscopic techniques. The DBDSC chelate binds to 99mTc with high efficiency at ambient temperature. The resulting chelate is stable under physiological conditions (37oC, pH=7.4) for at least 24 h after radiocomplexation. The receptor binding studies of 99mTc-[DTPA-bis(D-ser)] in established lung adeno carcinoma A549 exhibited Kd value to be 26nM. A549 Tumor in athymic mice was accumulated in the γ-images. The major accumulation of the radiotracer was observed in tumor, followed by kidneys. 99mTc-[DTPA-bis(D-ser)] has promising utility as SPECT-radiopharmaceutical.


Assuntos
Quelantes/síntese química , Neoplasias/diagnóstico por imagem , Compostos de Organotecnécio/síntese química , Compostos Radiofarmacêuticos/síntese química , Serina/síntese química , Pentetato de Tecnécio Tc 99m/síntese química , Tomografia Computadorizada de Emissão de Fóton Único , Animais , Quelantes/farmacocinética , Camundongos , Camundongos Endogâmicos BALB C , Camundongos Nus , Neoplasias/metabolismo , Compostos de Organotecnécio/farmacocinética , Coelhos , Ensaio Radioligante , Compostos Radiofarmacêuticos/farmacocinética , Serina/farmacocinética , Pentetato de Tecnécio Tc 99m/farmacocinética
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